fusidic acid [Ligand Id: 10815] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL374975 (Anhydrous fusidic acid, CEM-102, Fucidin caviject, Fucithalmic, Fusidate, Fusidic acid, NSC-56192, Ramycin, SQ 16,603, SQ-16603, Taksta) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
| ChEMBL | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.94 | pIC50 | 11500 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Taurocholate uptake in canalicular membrane vesicles of rat liver | F | 5.66 | pKi | 2200 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
| ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.76 | pIC50 | 17400 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of LTC4 uptake in Mrp2-expressing HEK cells | F | 4.89 | pKi | 13000 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
| ChEMBL | TP_TRANSPORTER: inhibition of E217betaG uptake in canalicular membrane vesicles of rat liver | F | 5.12 | pKi | 7600 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
| ChEMBL | TP_TRANSPORTER: inhibition of LTC4 uptake in canalicular membrane vesicles of rat liver | F | 5.26 | pKi | 5500 | nM | Ki | Biochem Pharmacol (2002) 64: 151-158 [PMID:12106615] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay | F | 4.23 | pIC50 | 59000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting | F | 4.23 | pIC50 | 59000 | nM | IC50 | Medchemcomm (2017) 8: 1152-1157 [PMID:30108825] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 infected in human RBC after 48 to 96 hrs by SYBR Green I dye-based fluorescence assay | F | 4.28 | pIC50 | 52800 | nM | IC50 | Medchemcomm (2015) 6: 2023-2028 |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 48 hrs | F | 4.28 | pIC50 | 52800 | nM | IC50 | Medchemcomm (2017) 8: 1152-1157 [PMID:30108825] |
| ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes after 48 hrs by giemsa staining based assay | F | 4.3 | pIC50 | 50000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840] |
| Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay | F | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840] |
| Plasmodium falciparum NF54 (target type: ORGANISM) [ChEMBL: CHEMBL2367131] | ||||||||
| ChEMBL | Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 infected in human RBC after 48 hrs by [3H]hypoxanthine incorporation assay | F | 4.23 | pIC50 | 59000 | nM | IC50 | Medchemcomm (2015) 6: 2023-2028 |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
